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1. 发明授权

US5968955A Disubstituted piperidine derivatives as neuroprotective agents 失效
标题翻译：二取代哌啶衍生物作为神经保护剂
公开(公告)号：US5968955A
公开(公告)日：1999-10-19
申请号：US43906
申请日：1998-03-31
申请人： Sergio Mantegani , Tiziano Bandiera , Manuela Villa , Mario Varasi , Carmela Speciale
发明人： Sergio Mantegani , Tiziano Bandiera , Manuela Villa , Mario Varasi , Carmela Speciale
IPC分类号： A61K31/00 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61P25/00 , A61P25/04 , C07D413/06
CPC分类号： C07D413/06
摘要： A Disubstituted piperidine compounds of formula (I), wherein R.sub.1 is hydrogen; bromo; chloro; a linear or branched C.sub.1 -C.sub.5 alkyl group; a linear or branched C.sub.1 -C.sub.5 alkoxy group; or an optionally substituted phenyl group; R.sub.2 is hydrogen, a linear or branched C.sub.1 -C.sub.5 alkyl group or an optionally substituted phenyl group; X is CH.sub.2, C.dbd.O, CHOH or C.dbd.NOH; R.sub.3 is hydrogen or a linear or branched C.sub.1 -C.sub.5 alkyl group; Y is a (CH.sub.2).sub.n group in which n is an integer from 0 to 4, CHOH, C.dbd.O or CH-A wherein A is an optionally substituted phenyl group; A is an optionally substituted phenyl group; W is hydrogen or hydroxy; stereoisomers thereof and their pharmaceutically acceptable salts. The compounds possess selective neuroprotective activity and are useful in the treatment of an acute or a degenerative CNS disease. A process is described for preparing the compounds and pharmaceutical compositions containing them.
摘要翻译： PCT No.PCT / EP95 / 04075第 371日期1998年3月31日 102（e）1998年3月31日PCT PCT 1996年9月16日PCT公布。公开号WO97 / 13769 日期1997年4月17日A式（I）的二取代哌啶化合物，其中R 1是氢; 溴氯直链或支链C 1 -C 5烷基; 直链或支链C 1 -C 5烷氧基; 或任选取代的苯基; R2是氢，直链或支链C1-C5烷基或任意取代的苯基; X是CH 2，C = O，CHOH或C = NOH; R3是氢或直链或支链C1-C5烷基; Y为（CH 2）n基团，其中n为0至4的整数，CHOH，C = O或CH-A，其中A为任选取代的苯基; A是任选取代的苯基; W是氢或羟基; 其立体异构体及其药学上可接受的盐。该化合物具有选择性神经保护活性，可用于治疗急性或退行性CNS疾病。描述了制备含有它们的化合物和药物组合物的方法。

2. 发明授权

US08173659B2 Substituted pyrazolo[4,3-C]pyridine derivatives active as kinase inhibitors 有权
标题翻译：作为激酶抑制剂活性的取代的吡唑并[4,3-C]吡啶衍生物
公开(公告)号：US08173659B2
公开(公告)日：2012-05-08
申请号：US13085889
申请日：2011-04-13
申请人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
发明人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
IPC分类号： A61K31/496 , A61K31/437
CPC分类号： C07D471/04
摘要： Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.
摘要翻译：公开了如本说明书中定义的式（I）的吡唑并[4,3-c]吡啶衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。

3. 发明授权

US6133302A 5-(3-Phenyl-3-oxo-propyl)-1H-tetrazole derivatives 失效
标题翻译： 5-（3-苯基-3-氧代 - 丙基）-1H-四唑衍生物
公开(公告)号：US6133302A
公开(公告)日：2000-10-17
申请号：US446895
申请日：1999-12-30
申请人： Paolo Pevarello , Antonio Giordani , Manuela Villa , Carmela Speciale , Mario Varasi
发明人： Paolo Pevarello , Antonio Giordani , Manuela Villa , Carmela Speciale , Mario Varasi
IPC分类号： A61K31/41 , A61P25/00 , A61P43/00 , C07D257/04
CPC分类号： C07D257/04
摘要： 5-(3-phenyl-3-oxo-propyl)-1H-tetrazole derivatives of formula (I) wherein each of R and R.sub.1, being the same or different, is hydrogen, halogen, hydroxy, trifluoromethyl, cyano, nitro, phenyl, benzyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, SOR.sub.4 or SO.sub.2 R.sub.4 wherein R.sub.4 is C.sub.1 -C.sub.6 alkyl, --N(R.sub.5 R.sub.6) in which each of R.sub.5 and R.sub.6 is, independently, hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 acyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl; R.sub.3 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl or a group --N(R.sub.7 R.sub.8) in which each of R.sub.7 and R.sub.8 is, independently, hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, phenyl, or one of R.sub.7 and R.sub.8 is hydrogen and the other is COR.sub.9 wherein R.sub.9 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl or a group --N(R.sub.10 R.sub.11) in which R.sub.10 and R.sub.11 are, each independently, hydrogen or C.sub.1 -C.sub.4 alkyl or, taken together, R.sub.2 and R.sub.3 form a carbocyclic C.sub.3 -C.sub.6 ring; and pharmaceutically acceptable salts thereof have kynurenine-3-hydroxylase enzyme inhibitory activity. ##STR1##
摘要翻译： PCT No.PCT / EP98 / 04032 Sec。 371 1999年12月30日第 102（e）1999年12月30日PCT PCT。1998年6月25日PCT公布。公开号WO99 / 02506 日本1月21日，19995-（3-苯基-3-氧代 - 丙基）-1H-四唑衍生物，其中R和R 1相同或不同，为氢，卤素，羟基，三氟甲基，氰基，硝基，苯基，苄基，C1-C6烷基，C1-C6烷氧基，C1-C6烷硫基，SOR4或SO2R4，其中R4是C1-C6烷基，-N（R5R6），其中R5和R6各自独立地为氢，C 1 -C 6烷基，甲酰基或C 2 -C 6酰基; R2是氢，C1-C6烷基，C1-C6烷氧基，苄基，苯基; R3是氢，羟基，C1-C6烷基，C1-C6烷氧基，苄基，苯基或基团-N（R7R8），其中R7和R8各自独立地是氢，C1-C4烷基，苄基，苯基或 R 7和R 8中的一个是氢，另一个是COR 9，其中R 9是氢，C 1 -C 4烷基，C 1 -C 4烷氧基，苯基或基团-N（R 10 R 11），其中R 10和R 11各自独立地是氢或C1- C4烷基或一起为R2和R3形成碳环C 3 -C 6环; 及其药学上可接受的盐具有犬尿氨酸-3-羟化酶抑制活性。

4. 发明申请

US20110230470A1 SUBSTITUTED PYRAZOLO[4,3-C]PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS 有权
标题翻译：作为激酶抑制剂活性的取代的吡唑并[4,3-C]吡啶衍生物
公开(公告)号：US20110230470A1
公开(公告)日：2011-09-22
申请号：US13085889
申请日：2011-04-13
申请人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
发明人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
IPC分类号： A61K31/551 , A61K31/496 , A61K31/437 , A61K31/5377 , A61P35/00 , A61P31/12 , A61P27/02 , A61P9/10 , A61P17/06 , A61P11/00 , A61P3/04 , A61P35/04 , A61P19/02 , A61P9/00 , A61P29/00 , A61N5/00
CPC分类号： C07D471/04
摘要： Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.
摘要翻译：公开了如本说明书中定义的式（I）的吡唑并[4,3-c]吡啶衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。

5. 发明授权

US07947686B2 Substituted pyrazolo[4,3-c]pyridine derivatives active as kinase inhibitors 有权
标题翻译：作为激酶抑制剂活性的取代的吡唑并[4,3-c]吡啶衍生物
公开(公告)号：US07947686B2
公开(公告)日：2011-05-24
申请号：US12096979
申请日：2006-12-06
申请人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
发明人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
IPC分类号： A61K31/496 , A61K31/437 , C07D401/14 , C07D471/04
CPC分类号： C07D471/04
摘要： Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.
摘要翻译：公开了如本说明书中定义的式（I）的吡唑并[4,3-c]吡啶衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。

6. 发明申请

US20090023745A1 Substituted Pyrazolo[4,3-c]Pyridine Derivatives Active as Kinase Inhibitors 有权
标题翻译：取代的吡唑并[4,3-c]吡啶衍生物作为激酶抑制剂
公开(公告)号：US20090023745A1
公开(公告)日：2009-01-22
申请号：US12096979
申请日：2006-12-06
申请人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
发明人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
IPC分类号： A61K31/496 , C07D471/04 , C07K14/71 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04
摘要： Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.
摘要翻译：公开了如本说明书中定义的式（I）的吡唑并[4,3-c]吡啶衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。

7. 发明申请

US20050004120A1 Arylmethyl-carbonylamino-thiazole derivatives and their use as antitumor agents 审中-公开
标题翻译：芳基甲基 - 羰基氨基 - 噻唑衍生物及其作为抗肿瘤剂的用途
公开(公告)号：US20050004120A1
公开(公告)日：2005-01-06
申请号：US10902326
申请日：2004-07-29
申请人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
发明人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
IPC分类号： C07D277/20 , A61K20060101 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/5377 , A61P20060101 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/08 , A61P19/02 , A61P25/28 , A61P31/12 , A61P35/00 , A61P37/02 , C07D20060101 , C07D277/04 , C07D277/46 , C07D401/00 , C07D417/12 , C07D417/14
CPC分类号： A61K31/426 , C07D277/46
摘要： A method of modulating apoptosis or treating diseases associated with protein kinases by administering to a mammal in need thereof of an effective amount of 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R1, R2 and R3 are as defined herein, or pharmaceutically acceptable salts thereof.
摘要翻译：通过向有需要的哺乳动物施用有效量的由式（I）或（II）表示的2-氨基-1,3-噻唑衍生物来调节凋亡或治疗与蛋白激酶相关的疾病的方法：其中R，R 1 ，R2和R3如本文所定义，或其药学上可接受的盐。

8. 发明授权

US06784198B1 Arylmethyl-carbonylamino-thiazole derivatives and their use as antitumor agents 失效
标题翻译：芳基甲基 - 羰基氨基 - 噻唑衍生物及其作为抗肿瘤剂的用途
公开(公告)号：US06784198B1
公开(公告)日：2004-08-31
申请号：US10048474
申请日：2002-07-18
申请人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
发明人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
IPC分类号： A61K31425
CPC分类号： A61K31/426 , C07D277/46
摘要： 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof are useful as, for example, the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
摘要翻译：由式（I）或（II）表示的2-氨基-1,3-噻唑衍生物：其中R，R 1，R 2和R 3在本文中定义，或其药学上可接受的盐可用作例如癌症的治疗，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病或神经变性疾病。

9. 发明授权

US6114365A Arylmethyl-carbonylamino-thiazole derivatives, process for their preparation, and their use as antitumor agents 有权
标题翻译：芳基甲基 - 羰基氨基 - 噻唑衍生物，其制备方法及其作为抗肿瘤剂的用途
公开(公告)号：US6114365A
公开(公告)日：2000-09-05
申请号：US372832
申请日：1999-08-12
申请人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
发明人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
IPC分类号： C07D277/20 , A61K20060101 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/5377 , A61P20060101 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/08 , A61P19/02 , A61P25/28 , A61P31/12 , A61P35/00 , A61P37/02 , C07D20060101 , C07D277/04 , C07D277/46 , C07D401/00 , C07D417/12 , C07D417/14
CPC分类号： A61K31/426 , C07D277/46
摘要： 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): ##STR1## where R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein, or pharmaceutically acceptable salts thereof, are useful in, for example, the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
摘要翻译：由式（I）或（II）表示的2-氨基-1,3-噻唑衍生物：其中R，R 1，R 2和R 3如本文所定义，或其药学上可接受的盐可用于例如癌症，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病或神经变性疾病。

10. 发明授权

US08470831B2 Acrylamido derivatives useful as inhibitors of the mitochondrial permeability transition 有权
标题翻译：丙烯酰胺衍生物可用作线粒体通透性转换的抑制剂
公开(公告)号：US08470831B2
公开(公告)日：2013-06-25
申请号：US13123852
申请日：2009-09-23
申请人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
发明人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
IPC分类号： A61K31/4965 , A61K31/445 , A61K31/4178 , A61K31/416 , A61K31/22 , A61K31/19 , A61K31/18 , A61K31/167 , C07D295/12 , C07D241/04 , C07D211/32 , C07D403/06 , C07D231/56 , C07D295/096 , C07C69/017 , C07C65/19 , C07C311/13 , C07C233/88
CPC分类号： C07C235/38 , C07C235/36 , C07C323/41 , C07C2601/04 , C07C2602/08 , C07D209/08 , C07D211/22 , C07D213/30 , C07D213/36 , C07D213/68 , C07D213/75 , C07D231/12 , C07D231/56 , C07D233/64 , C07D235/06 , C07D235/30 , C07D239/47 , C07D249/18 , C07D257/04 , C07D263/32 , C07D263/56 , C07D295/096 , C07D295/135 , C07D307/42
摘要： Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R′, R″, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
摘要翻译：可用作治疗剂的丙烯酰胺衍生物，特别是用于预防和/或治疗与线粒体通透性转换孔（MPTP）的活性相关的疾病和病症，例如以缺血/再灌注，氧化性或退行性组织损伤为特征的疾病，是在此描述。这些化合物属于结构式（I），其中R，R'，R“，W和a如说明书中所定义。本发明还涉及这些化合物的制备，以及包含它们的药物组合物。

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